Drug-conjugates, conjugation methods, and uses thereof
View Patent ↗In one aspect, an active agent-conjugate, methods of preparing the active agent-conjugate, and uses thereof is provided.
1. An active agent-conjugate, comprising Formula 1a:
or a pharmaceutically acceptable salt thereof,
wherein:
A is a targeting moiety selected from the group consisting of an antibody and an antibody fragment;
B is null;
X is N;
Y is N;
m is 1;
D is a drug;
L 2 is a linker independently selected from the group consisting of —(CH 2 ) n —, —(CH 2 CH 2 O) n , D-Val-Leu-Lys, Gly-Gly-Arg, and combinations thereof;
n is 1;
L is —NH—C(═O)—NH; and
L 1A is a linker selected from the group consisting of —(CH 2 ) n —, —(CH 2 CH 2 O) n , D Val-Leu-Lys, and Gly-Gly-Arg, or is null.
2. The active agent-conjugate of claim 1 wherein A is a monoclonal antibody (mAB).